在proline的cis-trans异构化打开了一个神经递质受入的离子通道孔
Sarah C R Lummis1, Darren L Beene, Lori W Lee
1Department of Biochemistry, University of Cambridge, Tennis Court Road, Cambridge CB2 1GA, UK.
Nature
|November 11, 2005
概括
5西胺3型 (5-HT3) 受体的受体.
科学领域:
- 神经科学是一个神经科学.
- 分子生物学分子生物学
- 结构生物学 结构生物学
背景情况:
- 5西胺3型 (5-HT3) 受体是Cys循环受体.
- 神经递质的结合通过未知的形状变化诱导离子通道门.
研究的目的:
- 阐明将神经递质结合与5-HT3受体中的通道关联系起来的机制.
- 为了研究一种特定的普罗林残留物 (Pro 8*) 在M2-M3循环中的作用.
主要方法:
- 不自然的氨基酸突变发生,以在8*位置上加入类型.
- 突变通道的功能性特征.
- 对M2-M3环进行核磁共振 (NMR) 研究.
主要成果:
- 支持变压器的烯类相应物导致了非功能通道.
- 在proline模拟的cis-trans能量和通道激活之间存在相关性.
- 核磁共振研究揭示了M2-M3循环的两个不同的结构形式.
结论:
- 8*的Cis-trans异构化作为5-HT3受体关门的分子开关.
- 这种异构化将神经递质结合与通道开通联系起来.
- M2-M3循环结构和Pro 8*对受体功能至关重要.
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